期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 19, 页码 9255-9261出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00420
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资金
- University of Bologna, FARB (FFBO) [125290]
- MIUR (PRIN)
- Fondazione Veronesi-Milano (Proj. Tryptoids)
Recently, the tryptophan-containing,noncationizable opioid peptides emerged with atypical structure and unexpected in vivo activity. Herein, we describe analogs of the naturally occurring mixed x/mu-ligand c[Phe-b-Pro-Phe-Trp] 1 (CJ-15,208). Receptor affinity, selectivity, and. agonism/ antagonism varied upon enlarging macrocycle size, giving the mu-agonist 9 or the delta-antagonist 10 characterized by low nanomolar affinity. In particular, the mu-agonist c[beta-Ala-D-Pro- Phe-Trp] 9 was shown to elicit potent antinociception in a mouse model of visceral pain upon systemic administration.
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